反应详情

6-[4-({4-[(5-Chloro-1H-indol-2-yl)sulphonyl]piperazin-1-yl}carbonyl)phenyl]-pyridazin-3-ol (see WO 99/57113, 0.054 gram, 0.11 mmol), 0.016 gram of anhydrous potassium carbonate (0.11 mmol, 1.0 eq.) and 0.02 gram of 1-bromo-2-(2-methoxy-ethoxy)ethane (0.11 mmol, 1.0 eq.) were mixed in 1.5 mL of dry N,N-dimethylform-amide. The mixture was treated with microwave at 150° C. for 1 hour. Without any work-up, purification was performed on preparative HPLC, which gave 0.023 gram of 6-{4-[4-(5-chloro-1H-indole-2-sulphonyl)-piperazine-1-carbonyl]-phenyl}-2-[2-(2-methoxy-ethoxy)-ethyl]-2H-pyridazin-3-one (yield 36%).

1. additionThe mixture was treated with microwave at 150° C. for 1 hour
2. customWithout any work-up, purification